Epigenetic Alterations in Renal Cell Cancer With TKIs Resistance: From Mechanisms to Clinical Applications

Li, Qinhan; Zhang, Zhenan; Fan, Yu; Zhang, Qian

doi:10.3389/fgene.2020.562868

Cited by 10 publications

(11 citation statements)

References 127 publications

(153 reference statements)

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“…Epigenetics modifications, such as DNA methylation, histone modifications, chromatin remodeling, and non‐coding RNA, can control the chromatin structure and influence gene expression without alterations in the DNA sequence 114 . Epigenetic modification plays an essential role in cancer biology, including drug resistance 115 …”

Section: Molecular Pathways Associated With Resistance To Treatment W...mentioning

confidence: 99%

“…A non‐coding RNA is an RNA molecule transcribed from RNA but not translated into a protein. 116 Micro RNA (miRNA), a particular class of non‐coding RNA, has been studied as a therapeutic target for TKI resistance in RCC 115 . Although an increasing number of studies have reported the potential role of miRNAs for TKI resistance in RCC as reviewed in depth, 117 there has been no reports of the clinical application of miRNA 118 .…”

Section: Molecular Pathways Associated With Resistance To Treatment W...mentioning

confidence: 99%

“…Overexpression of EZH2 enhances EMT by repression of E‐cadherin 123 . EZH2 is one of the central epigenetic mechanisms of TKI resistance in RCC 115 . Inhibition of EZH2 increased sensitivity to sunitinib in RCC cell lines 124 .…”

Section: Molecular Pathways Associated With Resistance To Treatment W...mentioning

confidence: 99%

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Molecular mechanisms of resistance to tyrosine kinase inhibitor in clear cell renal cell carcinoma

et al. 2022

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Clear cell renal cell carcinoma (ccRCC) is the most common subtype of renal cell carcinoma (RCC). Loss of von Hippel–Lindau tumor suppressor gene is frequently observed in ccRCC and increases the expression of hypoxia‐inducible factors and their targets, including epidermal growth factor, vascular endothelial growth factor, and platelet‐derived growth factor. Tyrosine kinase inhibitors (TKIs) offer a survival benefit in metastatic renal cell carcinoma (mRCC). Recently, immune checkpoint inhibitors have been introduced in mRCC. Combination therapy with TKIs and immune checkpoint inhibitors significantly improved patient outcomes. Therefore, TKIs still play an essential role in mRCC treatment. However, the clinical utility of TKIs is compromised when primary and acquired resistance are encountered. The mechanism of resistance to TKI is not fully elucidated. Here, we comprehensively reviewed the molecular mechanisms of resistance to TKIs and a potential strategy to overcome this resistance. We outlined the involvement of angiogenesis, non‐angiogenesis, epithelial‐mesenchymal transition, activating bypass pathways, lysosomal sequestration, non‐coding RNAs, epigenetic modifications and tumor microenvironment factors in the resistance to TKIs. Deep insight into the molecular mechanisms of resistance to TKIs will help to better understand the biology of RCC and can ultimately help in the development of more effective therapies.

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Section: Molecular Pathways Associated With Resistance To Treatment W...mentioning

confidence: 99%

Section: Molecular Pathways Associated With Resistance To Treatment W...mentioning

confidence: 99%

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Molecular mechanisms of resistance to tyrosine kinase inhibitor in clear cell renal cell carcinoma

et al. 2022

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“…Sunitinib, pazopanib, and cabozantinib are TKIs approved as first-line treatments, while axitinib and sorafenib are second-line treatments available for patients with RCC. However, 30% of patients are innately resistant to these treatments, and 70% of the initial responders acquire resistance in 2 years ( 17 , 18 ).…”

Section: Introductionmentioning

confidence: 99%

Precision Medicine: An Optimal Approach to Patient Care in Renal Cell Carcinoma

et al. 2022

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Renal cell cancer (RCC) is a heterogeneous tumor that shows both intra- and inter-heterogeneity. Heterogeneity is displayed not only in different patients but also among RCC cells in the same tumor, which makes treatment difficult because of varying degrees of responses generated in RCC heterogeneous tumor cells even with targeted treatment. In that context, precision medicine (PM), in terms of individualized treatment catered for a specific patient or groups of patients, can shift the paradigm of treatment in the clinical management of RCC. Recent progress in the biochemical, molecular, and histological characteristics of RCC has thrown light on many deregulated pathways involved in the pathogenesis of RCC. As PM-based therapies are rapidly evolving and few are already in current clinical practice in oncology, one can expect that PM will expand its way toward the robust treatment of patients with RCC. This article provides a comprehensive background on recent strategies and breakthroughs of PM in oncology and provides an overview of the potential applicability of PM in RCC. The article also highlights the drawbacks of PM and provides a holistic approach that goes beyond the involvement of clinicians and encompasses appropriate legislative and administrative care imparted by the healthcare system and insurance providers. It is anticipated that combined efforts from all sectors involved will make PM accessible to RCC and other patients with cancer, making a tremendous positive leap on individualized treatment strategies. This will subsequently enhance the quality of life of patients.

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“…Cancer is the pathological uncontrolled proliferation of the abnormal cells that divide rapidly [1]. Moreover, cancer can involve any tissue of the body and have many different forms in each body area [2,3].…”

Section: Introductionmentioning

confidence: 99%

5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation

et al. 2021

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A novel series of N-1 arylidene amino imidazole-2-thiones were synthesized, identified using IR, 1H-NMR, and 13C-NMR spectral data. Cytotoxic effect of the prepared compounds was carried out utilizing three cancer cell lines; MCF-7 breast cancer, HepG2 liver cancer, and HCT-116 colon cancer cell lines. Imidazole derivative 5 was the most potent of all against three cell lines. DNA flow cytometric analysis showed that, imidazoles 4d and 5 exhibit pre-G1 apoptosis and cell cycle arrest at G2/M phase. The results of the VEGFR-2 and B-Raf kinase inhibition assay revealed that compounds 4d and 5 displayed good inhibitory activity compared with reference drug erlotinib.

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Epigenetic Alterations in Renal Cell Cancer With TKIs Resistance: From Mechanisms to Clinical Applications

Cited by 10 publications

References 127 publications

Molecular mechanisms of resistance to tyrosine kinase inhibitor in clear cell renal cell carcinoma

Molecular mechanisms of resistance to tyrosine kinase inhibitor in clear cell renal cell carcinoma

Precision Medicine: An Optimal Approach to Patient Care in Renal Cell Carcinoma

5-Aryl-1-Arylideneamino-1H-Imidazole-2(3H)-Thiones: Synthesis and In Vitro Anticancer Evaluation

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